Structural modeling and analysis of the SARS-CoV-2 cell entry inhibitor camostat bound to the trypsin-like protease TMPRSS2 [0.03%]
与三肽基肽酶TMPRSS2结合的SARS-CoV-2细胞入侵抑制剂卡莫司他结构模型及分析
Diego E Escalante,David M Ferguson
Diego E Escalante
The type II transmembrane serine protease TMPRSS2 facilitates the entry of coronaviruses, such as SARS-CoV-2, into host cells by cleaving the S1/S2 interface of the viral spike protein. Based on structural data derived from X-ray crystallog...
In vitro and in vivo biological activities of azulene derivatives with potential applications in medicine [0.03%]
具有潜在医学应用价值的偶氮化合物的体内外生物活性研究
Paweł Bakun,Beata Czarczynska-Goslinska,Tomasz Goslinski et al.
Paweł Bakun et al.
Azulene is an aromatic hydrocarbon that possesses a unique chemical structure and interesting biological properties. Azulene derivatives, including guaiazulene or chamazulene, occur in nature as components of many plants and mushrooms, such...
Adenosine receptors as promising targets for the management of ocular diseases [0.03%]
腺苷受体有望成为眼部疾病的治疗靶点
Eleonora Spinozzi,Cecilia Baldassarri,Laura Acquaticci et al.
Eleonora Spinozzi et al.
The ocular drug discovery arena has undergone a significant improvement in the last few years culminating in the FDA approvals of 8 new drugs. However, despite a large number of drugs, generics, and combination products available, it remain...
Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery [0.03%]
氨基噻唑衍生物在抗癌药物发现中的研发和治疗潜力
Seyedeh Roya Alizadeh,Seyedeh Mahdieh Hashemi
Seyedeh Roya Alizadeh
Currently, the development of anticancer drug resistance is significantly restricted the clinical efficacy of the most commonly prescribed anticancer drug. Malignant disease is widely prevalent and considered to be the major challenges of t...
Gang Zhang,Li Sheng,Pooja Hegde et al.
Gang Zhang et al.
8-Nitrobenzothiazinones (BTZs) exemplified by macozinone are a new class of antitubercular agents with exceptionally potent activity. The aryl nitro group has been considered indispensable for activity since this is bioactivated within myco...
Synthesis and evaluation of benzenesulfonic acid derivatives as human neutrophil elastase (hNE) inhibitors [0.03%]
苯磺酸衍生物作为人中性粒细胞弹性蛋白酶抑制剂的合成与评估
Yanzhao Xu,Na Qi,Hui Wen et al.
Yanzhao Xu et al.
Herein we report our investigation concerning the development of Human neutrophil elastase (hNE) inhibitors for the treatment of Acute Respiratory Distress Syndrome (ARDS). Various benzenesulfonic acid derived compounds were synthesized and...
Synthesis of 4-oxotetrahydropyrimidine-1(2H)-carboxamides derivatives as capsid assembly modulators of hepatitis B virus [0.03%]
合成4-氧化四氢嘧啶-1（2H）羧酰胺衍生物作为乙肝病毒衣壳装配调节剂
Nicky Hwang,Haiqun Ban,Junjun Chen et al.
Nicky Hwang et al.
We report herein the synthesis and evaluation of phenyl ureas derived from 4-oxotetrahydropyrimidine as novel capsid assembly modulators of hepatitis B virus (HBV). Among the derivatives, compound 27 (58031) and several analogs showed an ac...
Yan Wang,Ruben Soto-Acosta,Rui Ding et al.
Yan Wang et al.
The AAA+ (ATPase associated with various cellular activities) protein p97, also called valosin-containing protein, is a hexameric ring ATPase and uses ATP hydrolysis to unfold or extract proteins from biological complexes. Many cellular pro...
Novel allosteric PARP1 inhibitors for the treatment of BRCA-deficient leukemia [0.03%]
新型异构PARP1抑制剂用于治疗BRCA缺陷的白血病
Elizabeth Hewlett,Monika Toma,Katherine Sullivan-Reed et al.
Elizabeth Hewlett et al.
The successful use of PARP1 inhibitors like olaparib (Loparza®) in the treatment of BRCA1/2- deficient breast cancer has provided clinical proof of concept for applying personalized medicine based on synthetic lethality to the treatment of...
Kaan Kucukoglu,Nagihan Faydalı,Dilek Bul
Kaan Kucukoglu
A disease emerged in the city of Wuhan, Hubei Province, Central China in the last month of 2019. It was pneumonia caused by a newly emerged coronavirus called COVID-19, later. Coronaviruses are enveloped RNA viruses belong to the Betacorona...